The disposition of the local anaesthetic, pentacaine, in rats and mice

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Abstract
The pharmacokinetics of pentacaine, a new local anaesthetic agent from the group of carbanilates, was investigated in the rat at a dose of 2 mg kg−1 i.v. and per os. A three‐compartment open model gave the best fit to the data. The model parameters are: t1/2 99.0 ± 14.1 min, Vss 7411.1 ml kg−1, Cl 77.9 ml min−1 kg−1; after oral administration t1/2 ab 4.9 ± 1.9 min, bioavailability 59.1 per cent, and extent of absorption 79.3 per cent. Pentacaine is eliminated almost entirely by metabolism. The metabolites are excreted equally in the urine and faeces at a relatively slow rate. The pharmacokinetics of pentacaine was linear in the dose range 0.008–4 mg kg−1. The whole‐body autoradiography in mice showed rapid transfer of 3H radioactivity from the vessels to tissues and a markedly heterogenous disposition pattern in organs.